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Minerva Biotecnologica 2006 September;18(3):153-7


language: English

In vitro anti-cancer property of five synthetic cantharidin analogues: a mini-review

Kok S. H. L. 1, Gambari R. 2, Chui C. H. 1, 3, Lam W. S. 1, Chen J. 1, Lau F. Y. 3, Wong R. S. M. 3, Cheng G. Y. M. 3, Lai P. B. S. 4, Leung T. W. T. 5, Chan A. S. C. 1, Tang J. C. O. 1

1 Cancer Drug Research and Development Laboratory Central Laboratory of the Institute of Molecular Technology for Drug Discovery and Synthesis and State Key Laboratory of Chinese Medicine and Molecular Pharmacology Shenzhen, China Department of Applied Biology and Chemical Technology The Hong Kong Polytechnic University;Hong Kong, P.R.China 2 ER-GenTech, Department of Biochemistry University of Ferrara, Ferrara, Italy 3 Department of Medicine and Therapeutics and 4 Department of Surgery, Prince of Wales Hospital The Chinese University of Hong Kong, Hong Kong, P.R China 5 Oncology Centre, The Hong Kong Sanatorium and Hospital Hong Kong, P.R.China


Novel drug discovery research for anti-cancer purposes remains urgent and essential, since cancer is still a major fatal cause disease in the 21st century. Cantharidin is a highly toxic compound especially affecting the haematopoietic and renal systems. It can be purified from some naturally occurring insects, including Mylabris species. Here we review our experience in the chemical synthesis and biological screening of five chemically modified cantharidin analogues on a series of human carcinoma cell lines. The pollination between chemical and bio-medical concepts during pharmaceutical design is encouraging in the discovery of novel compounds by maintaining the anti-cancer action, and simultaneously showing the selectivity on non-malignant cells.

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